C19 trityl and silyl andrographolide analogs exhibit in vitro anticancer activity in murine cancer models

Trityl ether C19 andrographolide analogs show nearly indistinguishable IC50 values of 4–20 M across murine melanoma, colorectal, neuroblastoma, and mammary carcinoma cell lines.

• Why it matters: Prior C19 silyl and trityl A-ring analogs showed improved anticancer activity in human cell lines, but their performance in murine adherent cancer models and signaling context remained unclear.
• What they did: The study tested C19 andrographolide analogs, including trityl and silyl ethers and a cyclic A-ring acetonide, for antiproliferative effects in B16F10, CT26, Neuro2a, and 4T1 cells, then assessed apoptosis by flow cytometry and probed Wnt1/{beta}-catenin modulation using CHIR-99021 and MSAB.
• The result: Compounds induced apoptosis to a greater extent than andrographolide, trityl ethers were generally more potent than C19 silyl ethers, and some silyl analogs caused cell cycle arrest without matching in vitro potency trends.

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